459836-30-7
中文名稱
[[[(1S)-1-(4-BROMOPHENYL)ETHYL]AMINO](1,2,3,4-TETRAHYDRO-2,3-DIOXO-5-QUINOXALINYL)METHYL] PHOSPHONIC ACID TETRASODIUM HYDRATE
英文名稱
PEAQX TETRASODIUM HYDRATE
CAS
459836-30-7
分子式
C34H32Br2N6Na4O11P2
分子量
1014.37
MOL 文件
459836-30-7.mol
459836-30-7 結(jié)構(gòu)式
基本信息
中文別名
化合物 PEAQX TETRASODIUM HYDRATE 英文別名
PEAQX TETRASODIUM HYDRATENVP-AAM077 tetrasodiuM hydrate
NVP-AAM 077 tetrasodiuM hydrate
[[[(1S)-1-(4-BROMOPHENYL)ETHYL]AMINO](1,2,3,4-TETRAHYDRO-2,3-DIOXO-5-QUINOXALINYL)METHYL] PHOSPHONIC ACID TETRASODIUM HYDRATE
物理化學(xué)性質(zhì)
密度1.639±0.06 g/cm3(Predicted)
儲存條件-20°C
酸度系數(shù)(pKa)1.19±0.10(Predicted)
形態(tài)Solid
顏色Light yellow to khaki
常見問題列表
生物活性
PEAQX (NVP-AAM077) tetrasodium hydrate 是有效的、選擇性的、口服有效的 NMDA 拮抗劑，其對 hNMDAR 1A 和 hNMDAR 2A 的 IC50 值分別為 270 nM 和 29600 nM。體外研究
PEAQX (3 μM) produces similar caspase-3 activation, while NVP-AAM007 is approximately three-fold more potent.
體內(nèi)研究
PEAQX (10-40 mg/kg) dose-dependently increased cortical caspase-3 activity following sub-chronic administration.
PEAQX (10 and 20 mg/kg) shows enhanced locomotor activity in response to PCP challenge (4 mg/kg on PN28-35) compared to saline pretreatment (F
3, 73
=4.99).
PEAQX (10 mg/kg, ip) antagonizes the effects of PRE084 on CaMKIV-TORC1-CREB and BDNF, even for learning and memory impairment.
| Animal Model: | Timed, day 14 pregnant female Sprague-Dawley rats. |
| Dosage: | 10, 20 or 40 mg/kg. |
| Administration: | S.C. |
| Result: | Showed a sensitized locomotor response to PCP challenge on PN28-35. |
| Animal Model: | Timed, day 14 pregnant female Sprague-Dawley rats. |
| Dosage: | 4 mg/kg. |
| Administration: | I.P. |
| Result: | Did not significantly increase locomotor activity in rats treated sub-chronically with PEAQX on PN7, 9 and 11. |
| Animal Model: | 11-week old C57BL/6 mice. |
| Dosage: | 10 mg/kg. |
| Administration: | IP. |
| Result: | Reversed the effect of PRE084 (F 3,78 = 10.446, p<0.01). |